Shown: posts 1 to 6 of 6. This is the beginning of the thread.
Posted by bleauberry on September 4, 2008, at 15:36:07
Could you please help me construct a list of medications that are 5ht1a autoreceptor antagonists? I don't want to go into long detail about why, just know that there is very good reason for it pertaining to my treatment. I am on the hunt for one that will specifically prevent 5ht1a from being excessively sensitive so as to allow enhanced transmission.
Since all meds have other actions, if you list a 5htt1a autoreceptor antagonist could you also please share what the other mechanisms of the med are? Some may be desired, neutral, ok, or bad, so that would be useful to know ahead of time.
I don't know about 5ht1a agonists or partial agonists, but if you do, please share. Anything that will wake up the receptors and keep them from oversensing too much serotonin when in fact there isn't enough.
Strange how this new insight came from a good reaction to the antibiotic Doxycycline. It gets complicated. To keep it short, 5ht1a is involved. I need to know what my choices are for that mechanism.
Thank you!
Posted by Phillipa on September 4, 2008, at 16:32:14
In reply to SLS and all....5ht1a autoreceptor antagonists...., posted by bleauberry on September 4, 2008, at 15:36:07
Can I follow as when on doxycylline felt better and wasn't sick at the time. Thanks Phillipa
Posted by ricker on September 4, 2008, at 16:42:52
In reply to SLS and all....5ht1a autoreceptor antagonists...., posted by bleauberry on September 4, 2008, at 15:36:07
Hi bleauberry,
Have you seen this drug chart?
http://www.slschofield.com/medicine/psychiatric_drugs_chart.html
I believe the link was previously provided by Scott?
I wish I could be of more help, but my knowledge is somewhat limited.
I quickly scrolled down the chart and noticed a few drugs that may meet you needs?
Regards, Rick
Posted by SLS on September 4, 2008, at 18:56:53
In reply to SLS and all....5ht1a autoreceptor antagonists...., posted by bleauberry on September 4, 2008, at 15:36:07
> Could you please help me construct a list of medications that are 5ht1a autoreceptor antagonists? I don't want to go into long detail about why, just know that there is very good reason for it pertaining to my treatment. I am on the hunt for one that will specifically prevent 5ht1a from being excessively sensitive so as to allow enhanced transmission.
1. pindolol - 5-HT1a somatodendritic autoreceptor antagonist; NE beta 1 receptor antagonist
> I don't know about 5ht1a agonists or partial agonists, but if you do, please share. Anything that will wake up the receptors and keep them from oversensing too much serotonin when in fact there isn't enough.
1. buspirone - 5-HT1a postsynaptic partial agonist; 5-HT1a autoreceptor full agonist; D2 receptor antagonist; NE alpha2 receptor antagonist (1-PP metabolite)2. gepirone - 5-HT1a postsynaptic partial agonist; 5-HT1a autoreceptor full agonist; NE alpha2 receptor antagonist (1-PP metabolite)
3. ipsapirone - 5-HT1a postsynaptic partial agonist; 5-HT1a autoreceptor full agonist; NE alpha2 receptor antagonist (1-PP metabolite)
4. flexinoxan - 5-HT1a postsynaptic partial agonist; 5-HT1a autoreceptor full agonist
* Repeated administration of milnacipran induces rapid desensitization of somatodendritic 5-HT1A autoreceptors but not postsynaptic 5-HT1A receptors
When you have a chance, I would love to know what you are on to...
- Scott
Posted by bleauberry on September 4, 2008, at 20:26:07
In reply to Re: SLS and all....5ht1a autoreceptor antagonists...., posted by SLS on September 4, 2008, at 18:56:53
SLS,Thanks, very helpful stuff.
You asked what I'm on. Nothing. But definitely need something. Doc wants me back on doxycycline as he suspects nervous system inflammation, unknown micro-organism infection, and my one day miracle response to it after feeling bad on it for 2 weeks. A common side effect of doxy in normal people is depression or mood swings, but there are reports of treatment resistant depression responding robustly to it. It is anti-inflammatory, antibacterial, and it somehow turns on the genes that instruct the 5ht1a autoreceptors to not be excessively sensitive. Weird, they are linking crib death to a genetic 5ht1a malfunction where it is to sensitive, resulting in lack of serotonin, and the resutling negative downstream effects on body temp, breathing, and heart function.Hey, pindolol looks perfect for me...theoretically that is. I've told docs many times it feels like when I start a reuptake inhibitor I feel improvement immediately, but within four days it feels like everything just shuts down and then I get worse and worse real fast. It's like I need the serotonin, it feels good, but as soon as the autoreceptors figure out what is going on, they say "no way", and turn everything off. That is exactly what it feels like and I've been through it so many times. Pindolol might prevent that, and in addition, the ne beta antagonism might improve the urinary muscle constrictions of milnacipran, which by a longshot has been my biggest promise in recent years.
I do not understand what an agonist would do. Would that further worsen an already over-sensitive receptor?
Also could you please explain to me what a "reverse agonist" is and how it works? When I see that term it confuses me.
Anyway, not sure where to go. I see a psych RN who is really good in 2 weeks. While her partner doctor is handling my physical stuff, he wants her to take over the mood stuff. Looks like Doxy is a definite, but I believe I will need more than that. The RN knows I respond fast to Ritalin and she is quite liberal with the pen, so she might just treat me symptomatically as I go through other physical treatments. No idea. My choice would be to endure the excruciation of Doxy for a couple weeks, see where it goes, and then decide. In the meantime I am fairly convinced my biggest help with me in receptor manipulation rather than neurotransmitter levels, so I am learning as much as I can to gear up for that attack. That's a new angle for me.
Thanks again for your help!
> 1. pindolol - 5-HT1a somatodendritic autoreceptor antagonist; NE beta 1 receptor antagonist
>
>
> > I don't know about 5ht1a agonists or partial agonists, but if you do, please share. Anything that will wake up the receptors and keep them from oversensing too much serotonin when in fact there isn't enough.
>
>
> 1. buspirone - 5-HT1a postsynaptic partial agonist; 5-HT1a autoreceptor full agonist; D2 receptor antagonist; NE alpha2 receptor antagonist (1-PP metabolite)
>
> 2. gepirone - 5-HT1a postsynaptic partial agonist; 5-HT1a autoreceptor full agonist; NE alpha2 receptor antagonist (1-PP metabolite)
>
> 3. ipsapirone - 5-HT1a postsynaptic partial agonist; 5-HT1a autoreceptor full agonist; NE alpha2 receptor antagonist (1-PP metabolite)
>
> 4. flexinoxan - 5-HT1a postsynaptic partial agonist; 5-HT1a autoreceptor full agonist
>
>
> * Repeated administration of milnacipran induces rapid desensitization of somatodendritic 5-HT1A autoreceptors but not postsynaptic 5-HT1A receptors
>
>
> When you have a chance, I would love to know what you are on to...
>
>
> - Scott
Posted by SLS on September 4, 2008, at 22:04:45
In reply to Re: SLS and all....5ht1a autoreceptor antagonists...., posted by bleauberry on September 4, 2008, at 20:26:07
> I do not understand what an agonist would do. Would that further worsen an already over-sensitive receptor?
I think being exposed to a stimulating ligand (whether it be the endogenous neurotransmitter or one synthesized as a drug) causes a downregulation of the receptor membranes - both pre- and post- synaptic. Sometimes, I get the idea that perhaps it doesn't matter which way you push the system, as long as the system is encouraged to reregulate itself. This would explain the apparant paradox of SSRIs and tianeptine.
> Also could you please explain to me what a "reverse agonist" is and how it works? When I see that term it confuses me.Inverse agonist.
An inverse agonist binds to a receptor, but does not stimulate it. In fact, it does just the opposite. It exerts a negative force upon neuronal activity. If a neural pathway is supposed to make you feel hot:
agonist - feel hot
antagonist - feel "not hot"
inverse agonist - feel coldThat's not the best example of the phenomenon, but I hope it helps a little.
- Scott
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